DNA Methyltransferase 1 Activity/Inhibitor Screening Assay Core Kit

Summary: Epigenetic inactivation of genes plays a critical role in many important human diseases, especially in cancer. A core mechanism for epigenetic inactivation of the genes is methylation of CpG islands in genome DNA. Methylation of CpG islands involves the course in which DNA methyltransferases (Dnmts) transfer a methyl group from S-adenosyl-L-methionine to the fifth carbon position of the cytosines. Four active Dnmts have been identified in mammals. They are named Dnmt1, Dnmt2, Dnmt3A, and Dnmt3B. Dnmt1 methylates cytosine residues, preferably in hemimethylated DNA. Mammalian Dnmt1 is believed to be involved in carcinogenesis, embryonic development, and several other biological functions. Hypermethylation by Dnmt1 is believed to inactivate the tumor suppressor genes leading to neoplastic transformation. The selective inhibition of Dnmt1 may lead to demethylation and expression of the silenced tumor suppressor genes. Thus, selective Dnmt1 inhibitors could be a new addition to cancer thera